deliveryofacetylthevetinbanantitumorcardiacglycosideusingpolymericmicellesforenhancedtherapeuticefficacyagainstlungcancercells
文献类型:期刊论文
作者 | Zhu Jingjing1; Zhang Xinxin2![]() ![]() |
刊名 | actapharmacologicasinica
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出版日期 | 2017 |
卷号 | 38期号:2页码:290 |
关键词 | cardiac glycoside acetylthevetin B antitumor lung cancer polymeric micelle drug delivery A549 xenograft tumor model |
ISSN号 | 1671-4083 |
DOI | 10.1038/aps.2016.113 |
英文摘要 | Acetylthevetin B (ATB), a cardiac glycoside from the seed of Thevetia peruviana (Pers) K Schum (yellow oleander), exhibits not only antitumor activity but also potential cardiac toxicity. In the present study, we attempted to enhance its antitumor action and decrease its adverse effects via chitosan-Pluronic P123 (CP) micelle encapsulation. Two ATB-loaded CP micelles (ATB-CP1, ATB-CP2) were prepared using an emulsion/solvent evaporation technique. They were spherical in shape with a particle size of 40-50 nm, showed a neutral zeta potential, and had acceptable encapsulation efficiency (>90%). Compared to the free ATB (IC_(50)=2.94 μmol/L), ATB-loaded CP micelles exerted much stronger cytotoxicity against human lung cancer A549 cells with lower IC_(50) values (0.76 and 1.44 μmol/L for ATB-CP1 and ATB-CP2, respectively). After administration of a single dose in mice, the accumulation of ATB-loaded CP1 micelles in the tumor and lungs, respectively, was 15.31-fold and 9.49-fold as high as that of free ATB. A549 xenograft tumor mice treated with ATB-loaded CP1 micelles for 21 d showed the smallest tumor volume (one-fourth of that in the control group) and the highest inhibition rate (85.6%) among all the treatment groups. After 21-d treatment, no significant pathological changes were observed in hearts and other main tissues. In summary, ATB may serve as a promising antitumor chemotherapeutic agent for lung cancer, and its antitumor efficacy was significantly improved by CP micelles, with lower adverse effects. |
语种 | 英语 |
源URL | [http://119.78.100.183/handle/2S10ELR8/288469] ![]() |
专题 | 中国科学院上海药物研究所 |
作者单位 | 1.Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Ji-nan University 2.中国科学院上海药物研究所 |
推荐引用方式 GB/T 7714 | Zhu Jingjing,Zhang Xinxin,Miao Yunqiu,et al. deliveryofacetylthevetinbanantitumorcardiacglycosideusingpolymericmicellesforenhancedtherapeuticefficacyagainstlungcancercells[J]. actapharmacologicasinica,2017,38(2):290. |
APA | Zhu Jingjing.,Zhang Xinxin.,Miao Yunqiu.,He Shufang.,Tian Danmei.,...&Gan Yong.(2017).deliveryofacetylthevetinbanantitumorcardiacglycosideusingpolymericmicellesforenhancedtherapeuticefficacyagainstlungcancercells.actapharmacologicasinica,38(2),290. |
MLA | Zhu Jingjing,et al."deliveryofacetylthevetinbanantitumorcardiacglycosideusingpolymericmicellesforenhancedtherapeuticefficacyagainstlungcancercells".actapharmacologicasinica 38.2(2017):290. |
入库方式: OAI收割
来源:上海药物研究所
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